| Reaction Details |
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 | Report a problem with these data |
| Target | Proto-oncogene tyrosine-protein kinase receptor Ret [G810R] |
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| Ligand | BDBM296748 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | RET G810R Mutant Assay |
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| IC50 | 159±n/a nM |
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| Citation |  Andrews, SW; Aronow, S; Blake, JF; Brandhuber, BJ; Cook, A; Haas, J; Jiang, Y; Kolakowski, GR; McFaddin, EA; McKenney, ML; McNulty, OT; Metcalf, AT; Moreno, DA; Tang, TP; Ren, L Substituted pyrazolo[1,5-A]pyridine compounds as RET kinase inhibitors US Patent US10172851 Publication Date 1/8/2019 |
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| More Info.: | Get all data from this article, Assay Method |
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| Proto-oncogene tyrosine-protein kinase receptor Ret [G810R] |
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| Name: | Proto-oncogene tyrosine-protein kinase receptor Ret [G810R] |
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| Synonyms: | CDHF12 | CDHR16 | PTC | Proto-oncogene tyrosine-protein kinase receptor Ret (G810R) | RET | RET Kinase (G810R) | RET kinase mutant (G810R) | RET51 | RET_HUMAN | ret enzyme (g810r) |
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| Type: | Enzyme Catalytic Domain |
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| Mol. Mass.: | 124418.43 |
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| Organism: | Homo sapiens (Human) |
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| Description: | P07949[G810R] |
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| Residue: | 1114 |
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| Sequence: | MAKATSGAAGLRLLLLLLLPLLGKVALGLYFSRDAYWEKLYVDQAAGTPLLYVHALRDAP
EEVPSFRLGQHLYGTYRTRLHENNWICIQEDTGLLYLNRSLDHSSWEKLSVRNRGFPLLT
VYLKVFLSPTSLREGECQWPGCARVYFSFFNTSFPACSSLKPRELCFPETRPSFRIRENR
PPGTFHQFRLLPVQFLCPNISVAYRLLEGEGLPFRCAPDSLEVSTRWALDREQREKYELV
AVCTVHAGAREEVVMVPFPVTVYDEDDSAPTFPAGVDTASAVVEFKRKEDTVVATLRVFD
ADVVPASGELVRRYTSTLLPGDTWAQQTFRVEHWPNETSVQANGSFVRATVHDYRLVLNR
NLSISENRTMQLAVLVNDSDFQGPGAGVLLLHFNVSVLPVSLHLPSTYSLSVSRRARRFA
QIGKVCVENCQAFSGINVQYKLHSSGANCSTLGVVTSAEDTSGILFVNDTKALRRPKCAE
LHYMVVATDQQTSRQAQAQLLVTVEGSYVAEEAGCPLSCAVSKRRLECEECGGLGSPTGR
CEWRQGDGKGITRNFSTCSPSTKTCPDGHCDVVETQDINICPQDCLRGSIVGGHEPGEPR
GIKAGYGTCNCFPEEEKCFCEPEDIQDPLCDELCRTVIAAAVLFSFIVSVLLSAFCIHCY
HKFAHKPPISSAEMTFRRPAQAFPVSYSSSGARRPSLDSMENQVSVDAFKILEDPKWEFP
RKNLVLGKTLGEGEFGKVVKATAFHLKGRAGYTTVAVKMLKENASPSELRDLLSEFNVLK
QVNHPHVIKLYGACSQDGPLLLIVEYAKYRSLRGFLRESRKVGPGYLGSGGSRNSSSLDH
PDERALTMGDLISFAWQISQGMQYLAEMKLVHRDLAARNILVAEGRKMKISDFGLSRDVY
EEDSYVKRSQGRIPVKWMAIESLFDHIYTTQSDVWSFGVLLWEIVTLGGNPYPGIPPERL
FNLLKTGHRMERPDNCSEEMYRLMLQCWKQEPDKRPVFADISKDLEKMMVKRRDYLDLAA
STPSDSLIYDDGLSEEETPLVDCNNAPLPRALPSTWIENKLYGMSDPNWPGESPVPLTRA
DGTNTGFPRYPNDSVYANWMLSPSAAKLMDTFDS
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| BDBM296748 |
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| n/a |
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| Name | BDBM296748 |
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| Synonyms: | US10112942, Example 483 | US10137124, Example 483 | US10172851, Example 483 | US10555944, Example 483 | US10953005, Example 483 |
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| Type | Small organic molecule |
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| Emp. Form. | C30H34N8O3 |
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| Mol. Mass. | 554.6428 |
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| SMILES | COc1ccc(CN2C3CC2CN(C3)c2ccc(cn2)-c2cc(OC[C@H](O)CN(C)C)cn3ncc(C#N)c23)cn1 |r| |
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| Structure | 
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